Synthesis of 1??(2, 4??dichlorophenyl)??4??cyano??5??(4??[11C] methoxyphenyl)??N??(piperidin??1??yl)??1H??pyrazole??3??carboxamide ([11C] JHU75528) and 1??(2?? …
…, HT Ravert, DP Holt, RF Dannals…
文献索引:Fan, Hong; Ravert, Hayden T.; Holt, Daniel P.; Dannals, Robert F.; Horti, Andrew G. Journal of Labelled Compounds and Radiopharmaceuticals, 2006 , vol. 49, # 12 p. 1021 - 1036
Abstract Two novel ligands for cerebral cannabinoid receptor (CB1), 1-(2, 4-dichlorophenyl)- 4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (JHU75528) and 1-(2-bromophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3- carboxamide (JHU75575) have been synthesized. Both JHU75528 and JHU75575 display a combination of higher binding affinity and lower lipophilicity than those of Rimonabant ( ...